Lytix Biopharma As

Pharmasum Therapeutics As

Peptide Patents As

Amicoat As

Wenche Stensen

John Sigurd Svendsen

Øystein Rekdal

Frederick Alan Leeson

Oystein Rekdal

Morten Bøhmer Strøm

Bengt Erik Haug

Merete Linchausen Skar

Istvan Marko

Roderick Alan Porter

Stig Olov Magnus Engqvist

Trond Flægstad

Bengt Erick Haug

ØYstein Rekdal

Morten Böhmer Ström

Trond Flaegstad

Stig Olov Engqvist

The present invention relates to a compound of formula (I) AA-AA-AA-R&#x2014;R(I) wherein, in any order, 2 of said AA (amino acid) moieties are cationic amino acids and 1 of said AA is an amino acid with a lipophilic R group, the R group having 14-27 non-hydrogen atoms; Ris a N atom, which may be substituted by a branched or unbranched C-Calkyl or aryl group, which group may incorporate up to 2 heteroatoms selected from N, O and S; and Ris an aliphatic moiety having 2-20 non-hydrogen atoms, said moiety being linear, branched or cyclic. The invention further relates to formulations containing these compounds, solid supports having these compounds attached thereto, the use of these compounds in therapy, particularly as antimicrobial, anti-tumour or anti-biofilm agents and non-therapeutic uses of these compounds, particularly their use in inhibiting biofilm formation or removing a biofilm.

Antimicrobial compounds

The present invention relates to compounds of Formula (I), which are DYRK1A and/or DYRK1B inhibitors, and their use in the treatment of neurodegenerative disorders such as Alzheimer's disease (AD) and Parkinson's disease (PD), metabolic disorders such as Metabolic Syndrome or diabetes mellitus, and cancer.

Benzothiazole derivatives as DYRK1 inhibitors

The present invention provides a compound of formula (I) wherein: Y represents a C or N atom which may be substituted or form a cyclic group with R&#x2033;' but may not be a quaternary C atom; R&#x2032; is &#x2014;OR, &#x2014;CONH, &#x2014;CF, F, &#x2014;OH, &#x2014;NO, &#x2014;CN or &#x2014;OCORin which R, is Calkyl and each may be in the beta or gamma position; R&#x2033; is Calkyl or H; and R&#x2033;&#x2032; is H or a group consisting of 1-12 non-hydrogen atoms and may be linear, branched and/or incorporate one or more cyclic groups, cyclic groups may be aromatic and/or heterocyclic and 2 or more cyclic groups may be linked or fused and each may be substituted; or a salt, hydrate or solvate of a compound of formula (I) for use in the treatment or prevention of a neurodegenerative disorder by inhibiting formation of neurofibrillary (tau) tangles and/or by inhibiting Dyrk 1A. The invention further relates to non-therapeutic uses of these compounds. 

Neurodegenerative therapies

The present invention relates to a compound of formula (I) AA-AA-AA-R&#x2014;R(I) wherein, in any order, 2 of said AA (amino acid) moieties are cationic amino acids and 1 of said AA is an amino acid with a lipophilic R group, the R group having 14-27 non-hydrogen atoms; Ris a N atom, which may be substituted by a branched or unbranched C-Calkyl or aryl group, which group may incorporate up to 2 heteroatoms selected from N, O and S; and Ris an aliphatic moiety having 2-20 non-hydrogen atoms, said moiety being linear, branched or cyclic. The invention further relates to formulations containing these compounds, solid supports having these compounds attached thereto, the use of these compounds in therapy, particularly as antimicrobial, anti-tumor or anti-biofilm agents and non-therapeutic uses of these compounds, particularly their use in inhibiting biofilm formation or removing a biofilm.

The present invention relates to a method of improving the resistance of a peptide or peptidomimetic to degradation by trypsin which comprises incorporating into said peptide or peptidomimetic a C-terminal capping group of formula (I): X&#x2014;Y&#x2014;Z (I) wherein X is a N atom, which may be substituted by a branched or unbranched C-Calkyl or aryl group which group may incorporate up to 2 heteroatoms selected from N, O and S; Y represents a group selected from &#x2014;R&#x2014;R&#x2014;, &#x2014;R&#x2014;R&#x2014;R,- and &#x2014;R&#x2014;R&#x2014;R&#x2014; wherein Ris C, O, S or N, and Ris C; each of Rand R, may be substituted by C-Calkyl groups or unsubstituted; and Z is a group comprising 1 to 3 cyclic groups each of 5 or 6 non-hydrogen atoms, 2 or more of the cyclic groups may be fused and one or more of the cyclic groups may be substituted; the Z. moiety incorporates a maximum of 15 non-hydrogen atoms; and wherein the bond between Y and Z is a covalent bond between Ror Rof Y and a non-hydrogen atom of one of the cyclic groups of Z.

Methods of peptide modification

The invention provides a method of treating tumors by adminstering to a human or animal patient an effective amount of a molecule of 2 to 4 amino acids or equivalent subunits in length, which incorporates a bulky and lipophilic group comprising at least 13 non-hydrogen atoms and containing no more than 2 polar functional groups, in which the bulky and lipophilic group incorporates one or more closed rings of 5 or more non-hydrogen atoms, and in which the molecule further has at least two more cationic than anionic moieties.

Method of treating tumors

The present invention relates to a peptide or peptidomimetic for use in the treatment of a biofilm-associated infection in a subject, wherein said peptide or peptidomimetic a) carries a net positive charge, &#x2014;b) is 1 to 6 amino acids in length or is an equivalently sized peptidomimetic; and c) is amphipathic in nature, having one or more lipophilic groups, one of said lipophilic groups comprising at least 7 non-hydrogen atoms.

Treatment of biofilms

The present invention relates to a compound of formula (I) AA-AA-AA-X&#x2014;Y&#x2014;Z wherein, in any order, 2 of said AA (amino acid) moieties are cationic amino acids and 1 of said AA is an amino acid with a lipophilic R group, the R group having 14-27 non-hydrogen atoms; X is a N atom, which may be substituted by a branched or unbranched C-Calkyl or aryl group which group may incorporate up to 2 heteroatoms selected from N, O and S; Y represents a group selected from &#x2014;R&#x2014;R&#x2014;, &#x2014;R&#x2014;R&#x2014;R&#x2014; and &#x2014;R&#x2014;R&#x2014;R&#x2014; wherein Ris C, O, S or N, and Ris C; each of Rand Rmay be substituted by C-Calkyl groups or unsubstituted; and Z is a group comprising 1 to 3 cyclic groups each of 5 or 6 non-hydrogen atoms, 2 or more of the cyclic groups may be fused and one or more of the cyclic groups may be substituted; the Z moiety incorporates a maximum of 15 non-hydrogen atoms; and wherein the bond between Y and Z is a covalent bond between Ror Rof Y and a non-hydrogen atom of one of the cyclic groups of Z. The invention further relates to formulations containing these compounds and their uses in therapy, particularly as antimicrobial or antitumoural agents.

The invention relates to the use of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto at least two bulky and lipophilic groups and having at least one more cationic than anionic moiety, in the manufacture of a medicament for destabilizing microbial cell membranes and the use as a membrane acting antimicrobial agent of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto a super bulky and lipophilic group comprising at least 9 non-hydrogen atoms and having at least two more cationic than anionic moieties and to methods of treatment involving such molecules, in particular peptides including peptide derivatives, and peptidomimetics.

Growing community of inventors

Kvaløysletta, Norway

Wenche Stensen